KR880013942A - Strong tricyclic oxazolone - Google Patents

Strong tricyclic oxazolone Download PDF

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Publication number
KR880013942A
KR880013942A KR1019880006306A KR880006306A KR880013942A KR 880013942 A KR880013942 A KR 880013942A KR 1019880006306 A KR1019880006306 A KR 1019880006306A KR 880006306 A KR880006306 A KR 880006306A KR 880013942 A KR880013942 A KR 880013942A
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South Korea
Prior art keywords
oxygen atom
integer
compound
pharmaceutically acceptable
group
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KR1019880006306A
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Korean (ko)
Inventor
디.죤스 윈톤
피.클락스톤 죠지
에이.슈네틀러 리차드
씨.데이지 리차드
Original Assignee
개리 디.스트릿
메렐 다우 파마슈티칼즈 인코포레이티드
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Application filed by 개리 디.스트릿, 메렐 다우 파마슈티칼즈 인코포레이티드 filed Critical 개리 디.스트릿
Publication of KR880013942A publication Critical patent/KR880013942A/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Cardiology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Laminated Bodies (AREA)
  • Non-Silver Salt Photosensitive Materials And Non-Silver Salt Photography (AREA)
  • Treatments For Attaching Organic Compounds To Fibrous Goods (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

The present invention relates to tricyclic oxazolones of the formula <CHEM> wherein Q is a divalent sulfur or oxygen atom; one of X and Z is an oxygen atom and the other is an imino group; and n is 0 or the integer 1 or 2, which enhance myocardial contractile force and are useful as cardiotonics in the treatment of heart failure.

Description

강심성 트리사이클릭 옥사졸론Strong tricyclic oxazolone

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음Since this is an open matter, no full text was included.

Claims (17)

하기일반식(Ⅰ)의 화합물 또는 이의 약제학적으로 허용되는 염.A compound of formula (I) or a pharmaceutically acceptable salt thereof. 상기식에서, Q는 2가의 황 또는 산소원자이고, X 및 Z 중 하나는 산소원자이고, 다른 하나는 이미노(NH)그룹이며, n은 0 이거나 1 또는 2의 정수이다.Wherein Q is a divalent sulfur or oxygen atom, one of X and Z is an oxygen atom, the other is an imino (NH) group, and n is 0 or an integer of 1 or 2. 제1항에 있어서, Q가 2가인 산소원자인 화합물.A compound according to claim 1, wherein Q is a divalent oxygen atom. 제1항 또는 2항에 있어서, n이 1 또는 2의 정수인 화합물.The compound of claim 1 or 2, wherein n is an integer of 1 or 2. 제1항 또는 2항에 있어서, X가 산소원자이며, Z는 아미노그룹인 화합물.3. A compound according to claim 1 or 2, wherein X is an oxygen atom and Z is an amino group. 제3항에 있어서, X가 산소원자이며, Z는 아미노그룹인 화합물.4. A compound according to claim 3, wherein X is an oxygen atom and Z is an amino group. 강심제로서 유효한양의 하기일반식(Ⅰ)의 화합물 또는 이의 약제학적으로 허용되는 염을 심부전증의 치료를 필요로 하는 환자에게 투여함을 포함하여, 상기 환자의 심부전증을 치료하는 방법.A method of treating heart failure in a patient comprising administering to a patient in need thereof a compound of formula (I) or a pharmaceutically acceptable salt thereof in an effective amount as a cardiac agent. 상기식에서, Q는 2가의 황 또는 산소원자이고, X 및 Z 중 하나는 산소원자이고, 다른 하나는 이미노(NH)그룹이며, n은 0 이거나 1 또는 2의 정수이다.Wherein Q is a divalent sulfur or oxygen atom, one of X and Z is an oxygen atom, the other is an imino (NH) group, and n is 0 or an integer of 1 or 2. 제6항에 있어서, Q가 2가인 산소원자인 방법.The method of claim 6, wherein Q is a divalent oxygen atom. 제6항 또는 2항에 있어서, n이 1 또는 2의 정수인 방법.The method of claim 6 or 2, wherein n is an integer of 1 or 2. 제6항 또는 2항에 있어서, X가 산소원자이며, Z는 아미노그룹인 방법.The method according to claim 6 or 2, wherein X is an oxygen atom and Z is an amino group. 제8항에 있어서, X가 산소원자이며, Z는 아미노그룹인 방법.The method of claim 8, wherein X is an oxygen atom and Z is an amino group. 유효량의 하기 일반식(Ⅰ)의 화합물 또는 이의 약제학적으로 허용되는 염을 심근수축력의 향상을 필요로 하는 환자에게 투여함을 포함하여, 상기 환자의 심근 수축력을 향상시키는 방법.A method of improving myocardial contractility in a patient, comprising administering an effective amount of a compound of Formula (I): or a pharmaceutically acceptable salt thereof to a patient in need thereof. 상기식에서, Q는 2가의 황 또는 산소원자이고, X 및 Z 중 하나는 산소원자이고, 다른 하나는 이미노(NH)그룹이며, n은 0 이거나 1 또는 2의 정수이다.Wherein Q is a divalent sulfur or oxygen atom, one of X and Z is an oxygen atom, the other is an imino (NH) group, and n is 0 or an integer of 1 or 2. 제11항에 있어서, Q가 2가인 산소원자인 방법.The method of claim 11, wherein Q is a divalent oxygen atom. 제11항 또는 2항에 있어서, n이 1 또는 2의 정수인 방법.The method of claim 11 or 2, wherein n is an integer of 1 or 2. 제11항 또는 2항에 있어서, X가 산소원자이며, Z는 아미노그룹인 방법.The method according to claim 11 or 2, wherein X is an oxygen atom and Z is an amino group. 제13항에 있어서, X가 산소원자이며, Z는 아미노그룹인 방법.The method of claim 13, wherein X is an oxygen atom and Z is an amino group. 하기일반식(Ⅰ)의 화합물 또는 이의 약제학적으로 허용되는 염 및 약제학적으로 허용되는 담체를 함유하는 약제학적 조성물.A pharmaceutical composition comprising a compound of formula (I): or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier. 상기식에서, Q는 2가의 황 또는 산소원자이고, X 및 Z 중 하나는 산소원자이고, 다른 하나는 이미노(NH)그룹이며, n은 0 이거나 1 또는 2의 정수이다.Wherein Q is a divalent sulfur or oxygen atom, one of X and Z is an oxygen atom, the other is an imino (NH) group, and n is 0 or an integer of 1 or 2. 하기일반식(2) 또는 (2')의 사이클릭 알파 아미노케톤의 수용액을 약 0℃ 내지 약 10℃에서, 약 2 내지 약 5몰 당량의 N,N'-카보닐디이미다졸과 반응시켜, 축합반응의 중간생성물을 분리시키고, 감압 및 150℃ 내지 약 200℃에서, 상기 축합반응 생성물을 약 5분 내지 약 30분 동안 가열한 다음 상기 생성물을 분리시킴을 포함하여, 하기일반식(Ⅰ)의 화합물 또는 이의 약제학적으로 허용되는 염을 제조하는 방법.An aqueous solution of the cyclic alpha aminoketone of the general formula (2) or (2 ') is reacted at about 0 ° C to about 10 ° C with about 2 to about 5 molar equivalents of N, N'-carbonyldiimidazole, The intermediate of the condensation reaction was separated and the condensation reaction product was heated at a reduced pressure and from 150 ° C. to about 200 ° C. for about 5 minutes to about 30 minutes, followed by separation of the product. A process for preparing a compound of the present invention or a pharmaceutically acceptable salt thereof. 상기식에서, Q는 2가의 황 또는 산소원자이고, X 및 Z 중 하나는 산소원자이고, 다른 하나는 이미노(NH)그룹이며, n은 0 이거나 1 또는 2의 정수이다.Wherein Q is a divalent sulfur or oxygen atom, one of X and Z is an oxygen atom, the other is an imino (NH) group, and n is 0 or an integer of 1 or 2. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019880006306A 1987-05-29 1988-05-28 Strong tricyclic oxazolone KR880013942A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US5548587A 1987-05-29 1987-05-29
US055,485 1987-05-29

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KR880013942A true KR880013942A (en) 1988-12-22

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EP (1) EP0293777B1 (en)
JP (1) JP2640671B2 (en)
KR (1) KR880013942A (en)
CN (1) CN1019116B (en)
AT (1) ATE83777T1 (en)
AU (1) AU600134B2 (en)
CA (1) CA1329601C (en)
DE (1) DE3876859T2 (en)
DK (1) DK290488A (en)
ES (1) ES2053621T3 (en)
FI (1) FI87075C (en)
GR (1) GR3007091T3 (en)
HU (1) HU198497B (en)
IL (1) IL86517A (en)
NO (1) NO882340L (en)
NZ (1) NZ224745A (en)
PH (1) PH25792A (en)
PT (1) PT87598B (en)
ZA (1) ZA883659B (en)

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* Cited by examiner, † Cited by third party
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US4762843A (en) * 1986-09-15 1988-08-09 Warner-Lambert Company Hetero [f] fused carbocyclic pyridines as dopaminergic agents
ATE141599T1 (en) * 1988-04-28 1996-09-15 Schering Corp CONDENSED POLYCYCLIC COMPOUNDS, COMPOSITIONS, METHOD OF PREPARATION AND USE THEREOF AS PAF ANTAGONIST, ANTHISTAMINIC AND/OR ANTI-INFLAMMATORY AGENTS
CN102696363A (en) * 2012-06-27 2012-10-03 莱恩农业装备有限公司 Anti-knife-jamming grass chopping mechanism
CN102696364A (en) * 2012-06-28 2012-10-03 莱恩农业装备有限公司 Grass chopping mechanism capable of automatically regulating stuck cutter

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Publication number Publication date
NO882340L (en) 1988-11-30
EP0293777A1 (en) 1988-12-07
PT87598B (en) 1995-03-01
EP0293777B1 (en) 1992-12-23
FI87075B (en) 1992-08-14
DK290488D0 (en) 1988-05-27
IL86517A (en) 1991-11-21
GR3007091T3 (en) 1993-07-30
CN88103236A (en) 1988-12-21
HUT47585A (en) 1989-03-28
NO882340D0 (en) 1988-05-27
IL86517A0 (en) 1988-11-15
DK290488A (en) 1988-11-30
CA1329601C (en) 1994-05-17
AU1662488A (en) 1988-12-01
PT87598A (en) 1989-05-31
FI882504A (en) 1988-11-30
CN1019116B (en) 1992-11-18
ES2053621T3 (en) 1994-08-01
DE3876859T2 (en) 1993-04-29
ZA883659B (en) 1989-01-25
FI87075C (en) 1992-11-25
DE3876859D1 (en) 1993-02-04
NZ224745A (en) 1990-09-26
AU600134B2 (en) 1990-08-02
ATE83777T1 (en) 1993-01-15
JPS6419080A (en) 1989-01-23
FI882504A0 (en) 1988-05-27
JP2640671B2 (en) 1997-08-13
PH25792A (en) 1991-11-05
HU198497B (en) 1989-10-30

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